Difference between revisions of "Imatinib (Gleevec)"
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==General information== | ==General information== | ||
− | Class/mechanism: Tyrosine kinase inhibitor, inhibits multiple tyrosine kinases, including Bcr-Abl tyrosine kinase, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML; the receptor tyrosine kinases for platelet-derived growth factor (PDGF), stem cell factor (SCF), and c-kit, which is the activating mutation found in gastrointestinal stromal tumor (GIST) tumors.<ref name="insert">[ | + | Class/mechanism: Tyrosine kinase inhibitor, inhibits multiple tyrosine kinases, including Bcr-Abl tyrosine kinase, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML; the receptor tyrosine kinases for platelet-derived growth factor (PDGF), stem cell factor (SCF), and c-kit, which is the activating mutation found in gastrointestinal stromal tumor (GIST) tumors.<ref name="insert">[https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/gleevec_tabs.pdf Imatinib (Gleevec) package insert]</ref><ref>[[Media:Imatinib.pdf | Imatinib (Gleevec) package insert (locally hosted backup)]]</ref><ref>[http://www.gleevec.com/ Gleevec manufacturer's website]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a |
Revision as of 18:03, 16 July 2016
General information
Class/mechanism: Tyrosine kinase inhibitor, inhibits multiple tyrosine kinases, including Bcr-Abl tyrosine kinase, the constitutively active tyrosine kinase resulting from the Philadelphia chromosome abnormality in CML; the receptor tyrosine kinases for platelet-derived growth factor (PDGF), stem cell factor (SCF), and c-kit, which is the activating mutation found in gastrointestinal stromal tumor (GIST) tumors.[1][2][3]
Route: PO
Extravasation: n/a
Fertility: evidence of harm [4]
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
- Acute lymphocytic leukemia
- Central nervous system (CNS) cancer
- Chronic myelogenous leukemia
- Hypereosinophilic syndrome
- Mast cell diseases
- Melanoma
- Gastrointestinal stromal tumor (GIST)
Patient drug information
- Imatinib (Gleevec) patient drug information (Chemocare)[5]
- Imatinib (Gleevec) patient drug information (UpToDate)[6]
History of changes in FDA indication
- 5/10/2001: Initial FDA approval "for the treatment of patients with chronic myeloid leukemia (CML) in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy."
- 2/1/2002: Additional indication "for the treatment of patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST)."
- 12/20/2002: Additional indication "for the treatment of newly diagnosed adult patients with Philadelphia chromosome positive chronic myeloid leukemia (CML).
- 5/20/2003: Additional indication "for the treatment of pediatric patients with Ph+ chronic phase CML whose disease has recurred after stem cell transplant or who are resistant to interferon alpha therapy."
- 10/19/2006: Additional indications for:
- "Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL)."
- "Adult patients with myelodysplastic/ myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene rearrangements."
- "Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-439 Kit mutation or with c-Kit mutational status unknown."
- "Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL) who have the FIP1L1-PDGFRα fusion kinase (mutational analysis or FISH demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRα fusion kinase negative or unknown."
- "Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP)."
- 1/25/2013: Additional indication for "Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL) in combination with chemotherapy."
Also Known As
CGP 57148, CGP57148B, Enliven, Glivec, Gleevac, Imalek, Imatib, Imatinib Mesilate, Imatinib Mesylate, STI-571, Temsan, Veenat.
References
- ↑ 1.0 1.1 Imatinib (Gleevec) package insert
- ↑ Imatinib (Gleevec) package insert (locally hosted backup)
- ↑ Gleevec manufacturer's website
- ↑ Pye SM, Cortes J, Ault P, Hatfield A, Kantarjian H, Pilot R, Rosti G, Apperley JF. The effects of imatinib on pregnancy outcome. Blood. 2008 Jun 15;111(12):5505-8. Epub 2008 Mar 5. link to original article PubMed
- ↑ Imatinib (Gleevec) patient drug information (Chemocare)
- ↑ Imatinib (Gleevec) patient drug information (UpToDate)
- Drug index
- Chemotherapy
- Oral chemotherapy
- Kinase inhibitors
- Bcr-Abl inhibitors
- KIT inhibitors
- PDGFR inhibitors
- Acute lymphocytic leukemia medications
- Central nervous system (CNS) cancer medications
- Chronic myelogenous leukemia medications
- Hypereosinophilic syndrome medications
- Mast cell diseases
- Melanoma medications
- Sarcoma medications
- Drugs FDA approved in 2001
- WHO Essential Cancer Medicine